title: Non-ionic surfactant vesicles simultaneously enhance antitumor activity and reduce the toxicity of cantharidin.
abstract: OBJECTIVE
  The objective of the present study was to prepare cantharidin-entrapped non-ionic surfactant vesicles (CTD-NSVs) and evaluate their potential in enhancing the antitumor activities and reducing CTD's toxicity.
  
  
  RESULTS
  CTD-NSVs were prepared by injection method. 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay and flow cytometry analysis showed that CTD-NSVs could significantly enhance in vitro toxicity against human breast cancer cell line MCF-7 and induce more significant cell-cycle arrest in G0/G1 phase. Moreover, Hoechst 33342 staining implicated that CTD-NSVs induced higher apoptotic rates in MCF-7 cells than free CTD solution. In vivo therapeutic efficacy was investigated in imprinting control region mice bearing mouse sarcoma S180. Mice treated with 1.0 mg/kg CTD-NSVs showed the most powerful antitumor activity, with an inhibition rate of 52.76%, which was significantly higher than that of cyclophosphamide (35 mg/kg, 40.23%) and the same concentration of free CTD (1.0 mg/kg, 31.05%). In addition, the acute toxicity and liver toxicity of CTD were also distinctly decreased via encapsulating into NSVs.
  
  
  CONCLUSIONS
  Our results revealed that NSVs could be a promising delivery system for enhancing the antitumor activity and simultaneously reducing the toxicity of CTD.
authors.affiliation: Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences, Beijing, PR China.
authors.forename: Wei
authors.initials: W
authors.lastname: Han
authors.forename: Shengpeng
authors.initials: S
authors.lastname: Wang
authors.forename: Rixin
authors.initials: R
authors.lastname: Liang
authors.forename: Lan
authors.initials: L
authors.lastname: Wang
authors.forename: Meiwan
authors.initials: M
authors.lastname: Chen
authors.forename: Hui
authors.initials: H
authors.lastname: Li
authors.forename: Yitao
authors.initials: Y
authors.lastname: Wang
mesh_terms: D000704:Analysis of Variance; D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology / Q000633:toxicity; D017209:Apoptosis / Q000187:drug effects; D002193:Cantharidin / Q000737:chemistry / Q000494:pharmacology / Q000633:toxicity; D002453:Cell Cycle / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D004337:Drug Carriers / Q000737:chemistry* / Q000633:toxicity; D006801:Humans; D057927:Hydrophobic and Hydrophilic Interactions; D061986:MCF-7 Cells; D008297:Male; D051379:Mice; D008813:Mice, Inbred ICR; D013501:Surface-Active Agents / Q000737:chemistry* / Q000633:toxicity; D023041:Xenograft Model Antitumor Assays
chemical_list: D000970:Antineoplastic Agents; D004337:Drug Carriers; D013501:Surface-Active Agents; D002193:Cantharidin
keywords: antitumor activity; cantharidin; non-ionic surfactant vesicle; toxicity